Colchicine-like β-acetamidoketones as inhibitors of microtubule polymerization: Design, synthesis and biological evaluation of in vitro anticancer activity.

ABSTRACT:

Objectives

In this study a series of novel colchicine-like β-acetamidoketones was designed and synthesized as potential tubulin inhibitors.

Materials and methods

The cytotoxicity of the novel synthesized β-acetamidoketones was assessed against two cancerous cell lines including MCF-7 (human breast cancer cells) and A549 (adenocarcinomic human alveolar basal epithelial cells) employing the MTT test. Tubulin polymerization test was done by using a commercial kit (tubulin polymerization assay kit).

Results

In general, the cytotoxicity activities were highly dependent on the aromatic substitution pattern of phenyl ring at β position of β-acetamidoketones. Based upon, compound 4f possessing the same structural elements of colchicine and chalcone 1, revealed the most

SUBMITTER: Karimikia E 

PROVIDER: S-EPMC6885397 | biostudies-literature | 2019 Oct

REPOSITORIES: biostudies-literature